• 제목/요약/키워드: 3-Hydroxy-3-methylglutaryl-coenzyme A reductase

검색결과 66건 처리시간 0.023초

Hypocholesterolemic Effect of Amaranth Squalene (Amaranth esculantus) in Rats Fed a High Cholesterol Diet

  • Kim, Hye-Kyung;Chang, Young-Jeong;Heo, Ho-Jin;Cho, Hong-Yon;Hong, Bum-Shik ;Shin, Dong-Hoon
    • Preventive Nutrition and Food Science
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    • 제8권1호
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    • pp.13-18
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    • 2003
  • In experiment 1, rats (n=6) fed diet containing 10 g/kg cholesterol for 4 wk (control) with either no amaranth (control), amaranth grain (300 g/kg, AG) or amaranth oil (90 g/kg, AO). Both the AG and AO groups had lower concentration of serum and hepatic cholesterol and triglyceride than the controls (p < 0.05). Fecal excretions of cholesterol and bile acid in AO group increased about 4 fold and 2 fold, respectively, while AG affected only bile acid excretion (p < 0.05). In experiment 2, rats (n=6) were fed the cholesterol diet for 4 wk and injected intraperitoneally with saline (control) or amaranth squalene (AS) for 7d. The hypolipidemic effect of AS was evident in both serum and liver. Fecal excretions of cholesterol and bile acid were greater (p < 0.05) in AS than control. HMG-CoA (3-hydroxy-3-methylglutaryl coenzyme A) reductase activity was reduced in AS group (11.6%, p=0.13). This study suggests that the cholesterol-lowering effect of AS is mediated by greater fecal elimination of steroids through interference with cholesterol absorption.

페놀 화합물로부터 HMG-CoA reductase 저해 활성 물질 탐색 (Screening of Phenolic Compounds with Inhibitory Activities against HMG-CoA Reductase)

  • 손건호;이주연;이정순;강삼식;손호용;권정숙
    • 생명과학회지
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    • 제27권3호
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    • pp.325-333
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    • 2017
  • 심혈관계 질환은 질환별 사망률 순위에 있어서 세계에서는 1위이며, 우리나라에서는 2위인 질병이다. 심혈관계 질환 발생의 주 위험 요인인 콜레스테롤은 HMG-CoA reductase에 의해 간에서 신생합성이 조절된다. 현재 고콜레스테롤혈증 치료에 statin이 널리 사용되고 있지만 광범위한 부작용이 보고되고 있어서 이를 대체하거나 보조할 수 있는 천연물 유래의 기능성 물질 개발이 필요한 실정이다. 따라서 본 연구에서는 혈장 콜레스테롤 감소 활성을 가지는 물질을 발굴하고자 71종의 페놀 및 그와 관련된 화합물들을 대상으로 10ug/ml 농도에서 HMG-CoA reductase 저해 활성을 탐색하였다. 그 결과, 1,4-naphthoquinone의 HMG-CoA reductase 저해율이 99.4%로 가장 높았고, 다음으로 plumbagin 91.4%, pentagalloyl ${\beta}-D-glucose$ 46.6%, 2,4-dihydroxybenzoic acid 40.9%, shikonin 37.7%, 1,2-naphthoquinone 36.6%, trans-cinnamic acid 32.0%, acetonylgeraniin 30.2%, benzoic acid 28.5%, geraniin 28.3%, gentisic acid 22.3%의 순이었다. $IC_{50}$값을 계산한 결과, 1,4-naphthoquinone가 $2.1{\mu}g/ml$로 가장 낮았으며, plumbagin과 pentagalloyl ${\beta}-D-glucose$은 각각 $5.8{\mu}g/ml$$13.1{\mu}g/ml$으로 나타났다. 1,4-naphthoquinone과 plumbagin의 경우, $5{\mu}g/ml$에서도 각각 90.3%와 43.3%의 저해율을 나타내었다.

한방약물로부터 항고지혈증 치료약물개발(I) -수종 한약재의 항고지혈증 활성검색- (Studies on the Development of Antihyperlipidemic Drugs from Oriental Herbal Medicines(I) -Antihyperlipidemic Activities of Oriental Herbal Medicines-)

  • 정은아;김동현;이상인;김남재
    • 생약학회지
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    • 제30권4호
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    • pp.368-376
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    • 1999
  • Twenty-four Oriental herbal medicines including Platycodi Radix and Scutellariae Radix, etc., which have been used for the cure of hyperlipidemia, coronary heart, disease were evaluated for the 3-hydroxy-3-methylglutaryl coenzyme A(HMG-CoA) reductase inhibition and antioxidant effect on a free radical, 1,1-diphenyl-2-picrylhydrazyl(DPPH) in vitro, and antihyperlipidemic effect on hyperlipidemic rats induced by Triton WR-1339 in vivo. 80% MeOH extract of eight herbs including Scutellariae Radix, Coptidis Rhizoma, Paeoniae Radix Rubra, Moutan Cortex Radicis, Angelicae Gigantis Radix, Bambusae Caulis in Taeniam, Cinnamomi Ramulus and Crataegi Fructus inhibited the HMG-CoA reductase activities and exhibited a radical-trapping action on a stable free radical, DPPH. On Triton WR-1339-induced hyperlipidemic rats, four herbs including Scutellariae Radix, Angelicae Gigantis Radix, Bambusae Caulis in Taeniam and Cinnamomi Ramulus showed respectively the significant suppression of serum total cholesterol, triglyceride, phospholipid and LDL-cholesterol levels and serum transaminase(ALT and AST) activities. From these results, it is suggested that each 80% MeOH extract of Scutellariae Radix, Angelicae Gigantis Radix, Bambusae Caulis in Taeniam and Cinnamomi Ramulus have effective antihyperlipidemic action against hyperlipidemia.

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Lactobacillus plantarum DR7 Reduces Cholesterol via Phosphorylation of AMPK That Down-regulated the mRNA Expression of HMG-CoA Reductase

  • Lew, Lee-Ching;Choi, Sy-Bing;Khoo, Boon-Yin;Sreenivasan, Sasidharan;Ong, Kee-Leong;Liong, Min-Tze
    • 한국축산식품학회지
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    • 제38권2호
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    • pp.350-361
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    • 2018
  • Hypercholesterolemia is one of the primary risk factors for cardiovascular diseases. The use of lactobacilli probiotics to reduce blood cholesterol levels have been extensively reported. However, more information is needed to evaluate the possible mechanisms involved and to identify possible targets for further therapeutic development. In this study, strains of lactobacilli were screened based on the ability to assimilate cholesterol, and prevention of cholesterol accumulation in hepatic (HepG2) and intestinal (HT-29) cells. Cell free supernatant (CFS) from Lactobacillus plantarum DR7 showed a higher ability to assimilate cholesterol, reduction in cholesterol accumulation in both HepG2 and HT-29 cells, accompanied by reduced mRNA expression of HMG-CoA reductase (HMGCR) in HepG2 (p<0.05), compared to other lactobacilli. The reduction of HMGCR expression was also diminished in the presence of an AMPK inhibitor (Compound C), suggesting that L. plantarum DR7 exerted its effect via the AMPK pathway, typically via the phosphorylation of AMPK instead of the AMPK mRNA expression in HepG2 (p<0.05). Altogether, our present study illustrated that lactobacilli could exert cholesterol lowering properties along the AMPK pathway, specifically via phosphorylation of AMPK that led to reduced expression of HMGCR.

플라보노이드 화합물로부터 HMG-CoA reductase 저해 활성 물질 탐색 (Screening of Flavonoid Compounds with HMG-CoA Reductase Inhibitory Activities)

  • 손건호;이주연;이정순;강삼식;손호용;권정숙
    • 생명과학회지
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    • 제28권2호
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    • pp.247-256
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    • 2018
  • 심혈관계 질환은 질환별 사망률 순위에 있어서 세계에서는 1위이며, 우리나라에서는 2위인 질병이다. 심혈관계 질환 발생의 주 위험 요인인 콜레스테롤은 HMG-CoA reductase에 의해 간에서 신생합성이 조절된다. 현재 고콜레스테롤혈증 치료에 statin이 널리 사용되고 있지만 광범위한 부작용이 보고되고 있어서 이를 대체하거나 보조할 수 있는 천연물 유래의 기능성 물질 개발이 필요한 실정이다. 따라서 본 연구에서는 혈장 콜레스테롤 감소 활성을 가지는 물질을 발굴하고자 98종의 플라보노이드 및 그와 관련된 화합물들을 대상으로 $10{\mu}g/ml$ 농도에서 HMG-CoA reductase 저해 활성을 탐색하였다. 그 결과, sophoraflavanone G, morin, 및 kuraridin이 각각 54.6%, 45.04% 및 21.9%의 저해활성을 타내었으며, $IC_{50}$값을 계산한 결과, sophoraflavanone G가 $7.3{\mu}g/ml$로 가장 낮았으며 morin과 kuraridin은 각각 $13.3{\mu}g/ml$$87.4{\mu}g/ml$으로 확인되어, 향후 고콜레스테롤혈증 예방 및 치료제의 가능성을 제시하였다.

Effects of Methanol Extract of Prosomillet on Cholesterol and Fatty Acid Metabolism in Rat

  • Cho, Sung-Hee;Jung, Seung -Eun;Lee, Hye-Kyung;Ha, Tae-Youl
    • Preventive Nutrition and Food Science
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    • 제4권3호
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    • pp.188-192
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    • 1999
  • To study effects of methanol extract of prosomillet on lopid metabolism , five groups of male Sprang-Dawley rats weighing 116$\pm$9 g were fed test diets for four weeks. The five diets consisted of one low fat(5% w/w) diet containing starch as carbohydrate source(normal) and four high fat diets(15% w/w) containing 40.5%(w/w)sucrose(control) and additional 80% nethanol extractof prosomillet at the levels of 0.3% and 1%(w/w) or prosomillet powder at the level of 20%(w/w). Serum level of total cholesterol was a little higher but that of triglyceride was 41% lower in 20% (w/w) prosomillet powder group than in the control group. The cholesterol levels of two Liver cholesterol levels were lower and phospolipid levels higher in all three prosomillet powder group . Fecal excretionof bile acid was most increased in the prosomillet powder group among all five test groups. Acitivity of liver microsomal 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase was significantly lower in 0.3% methanol extract fed group than the control and also appeared to be reduced in 1% extract fed one, wherease those of 20 cholesterol 7$\alpha$-hydroxylase were not different among the five groups. Activities of liver cytosilic glucose-6-phosphate dehydrogenase(G6PDH) and malic enzyme were decreased in 0.3% prosomillet methanol extract and 20% powder groups. The results indicate that in addition to fiber, certain active components in prosomillet have potential to exert hypolipidemic effects via regulating hepatic cholesterogenesis and lipogenesis.

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쌍강탕(雙降湯)이 고(高)cholesterol 식이(食餌)로 유발(誘發)된 고지혈증(高脂血症) 백서(白鼠)에 미치는 영향(影響) (The Effects of Ssanggang-tang($Shu\bar{a}ngji\grave{a}ng-t\bar{a}ng$) on Rat with Induced Hyperlipidemia)

  • 이재휘;임승민;안정조;조현경;김윤식;설인찬;유호룡
    • 대한한방내과학회지
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    • 제29권2호
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    • pp.432-442
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    • 2008
  • Objective : Ssanggang-tang(SGT) is noted as an effective method to treat hyperlipidemia in China. The main purpose of this study was analysis of the effects of Ssanggang-tang(SGT) on rats induced with caused hyperlipidemia. Methods : We observed 3 experimental groups: normal, control, and SGT. Rats were provided a normal diet in the normal group, and the other groups were provided a hyperlipidemic diet to induce hyperlipidemia. After 2 weeks, SGT was treated in the SGT group. For 6 weeks, values related to hyperlipidemia were observed in the 3 experimental groups. Results : SGT decreased some values related to hyperlipidemia like total cholesterol, low density lipoprotein cholesterol(LDL cholesterol), triglyceride, acetocoenzyme A acetyltransferase(ACAT), and 3-hydroxy-3-methylglutaryl coenzyme A reductase(HMG-CoA reductase). However, it showed no effect on weight change or high density lipoprotein cholesterol(HDL cholesterol). Conclusion : These results suggest that SGT might be effective in treatment and prevention of hyperlipidemia.

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The Risk of Rosacea According to Chronic Diseases and Medications: A 5-Year Retrospective, Multi-Institutional Case-Control Study

  • Son, Jee Hee;Chung, Bo Young;Jung, Min Je;Choi, Yong Won;Kim, Hye One;Park, Chun Wook
    • Annals of dermatology
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    • 제30권6호
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    • pp.676-687
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    • 2018
  • Background: Rosacea is associated with chronic systemic disease. However, research is lacking in Asian countries. Objective: To evaluate the association between rosacea and cardiovascular diseases (CVDs) related systemic comorbidities, and the use of antihypertensive and antihyperlipidemic drugs in Korea. Methods: A five-year retrospective study, using hospital database, was conducted in five medical centers for five years. Totally 1,399,528 patients were evaluated. Results: The overall frequency for diagnosed rosacea was 0.18% over five years (2,536 rosacea patients). Patients with diabetes and patients with dyslipidemia were more likely to have rosacea (odd ratio [OR] 2.724, 95% confidence interval [CI] 1.295~5.730, p=0.016; OR 1.788, 95% CI 1.445~2.212, p<0.001). Patients with CVD were less likely to have rosacea (OR 0.431, 95% CI 0.244~0.760, p=0.003). Patients with ${\alpha}$-blocker prescriptions and patients with ${\beta}$-blocker prescriptions showed a tendency diagnosed with rosacea frequently (OR 1.963, 95% CI 1.200~3.212, p=0.006; OR 3.939, 95% CI 3.512~4.419, p<0.001). Patients with [beta]-hydroxy-[beta]-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, and those with fibrate, were prone to have rosacea (OR 1.599, 95% CI 1.390~1.839, p<0.001; OR 1.660, 95% CI 1.056~2.609, p=0.026). As adjusted results, among the patients who took HMG-CoA reductase inhibitor without dyslipidemia, rosacea was less likely to be diagnosed (OR 0.780, 95% CI 0.620~0.982, p=0.034). Conclusion: Rosacea is associated with chronic diseases and drugs.

Anti-aging Effect and Gene Expression Profiling of Aged Rats Treated with G. bimaculatus Extract

  • Ahn, Mi Young;Hwang, Jae Sam;Yun, Eun Young;Kim, Min-Ji;Park, Kun-Koo
    • Toxicological Research
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    • 제31권2호
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    • pp.173-180
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    • 2015
  • Extract from Gryllus bimaculatus crickets inhibits oxidation at the DNA level, with reduced production of 8-hydroxy-2'-deoxyguanosine (8-OHdG). Microarray analyses were performed with a rat 28K cDNA clone set array to identify the gene expression profiles of aged (10 months old) Wistar Kyoto rats treated for one month with 100 mg/kg G. bimaculatus ethanol extract to assess the effects. The extract produced a meaningful anti-edema effect, evident by the inhibition of creatinine phosphokinase activity. The weights of abdominal and ovarian adipose tissues were reduced and the proportion of unsaturated fatty acids in adipose tissues was increased in an extract dose-dependent manner. Compared with untreated control rats, rats treated with the extract displayed the upregulation of 1053 genes including Fas (tumor necrosis factor receptor superfamily, member 6), Amigo3 (adhesion molecule with an immunoglobulin-like domain), Reticulon 4, 3-hydroxy-3-methylglutaryl-coenzyme (Hmgcr; a reductase), related anti-fatigue (enzyme metabolism), and Rtn antioxidant, and the downregulation of 73 genes including Ugt2b (UDP glycosyltransferase 2 family), Early growth response 1, and Glycoprotein m6a. Data suggest that G. bimaculatus extract may have value in lessening the effects of aging, resulting in a differential gene expression pattern indicative of a marked stress response and lower expression of metabolic and biosynthetic genes.

3T3-L1 전지방세포에서 발효 삼정환의 지방 분화 억제 효과 (Effect of Probiotics-Fermented Samjunghwan on Differentiation in 3T3-L1 Preadipocytes)

  • 송미영;;김호준
    • 한국식품영양과학회지
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    • 제42권1호
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    • pp.1-7
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    • 2013
  • 본 연구에서는 3T3-L1 전지방세포를 이용하여 발효 삼정환의 지방 분화 억제 효과를 확인하고자 하였다. 삼정환을 5가지 주요 유산균으로 각각 발효시킨 후, Oil Red O 염색법으로 지방세포 분화 억제 여부를 알아보고, 이의 기전을 알기 위해서 지방생성에 핵심적인 역할을 하는 transcription factor 및 지질 조절 효소의 유전자 발현량을 비교하여 보았다. Oil Red O 염색 분석에서는 Lactobacillus plantarum, Enterococcus faecium으로 발효한 삼정환에서 지방구 수의 감소를 확인할 수 있었다. 또한 transcription factor로 $C/EPB{\alpha}$, $PPAR{\gamma}$, UCP-2 및 콜레스테롤 조절과 관련된 효소인 HMG-CoA reductase의 4가지 유전자 발현 정도를 분석하였는데, 발효시키지 않은 삼정환의 경우 농도가 $100{\mu}L/mL$ 이상일 때 네 가지 항목에서 억제 효과를 나타냈으며, 발효시켰을 때는 유산균의 종류에 따라 효과 억제효과가 있었는데, Lactobacillus plantarum으로 발효한 삼정환이 효과가 가장 좋은 것으로 나타났다. Lactobacillus plantarum으로 발효한 삼정환은 동일 농도의 발효하지 않은 삼정환과 비교했을 때, Oil Red O 실험에서 염색된 지방구 수가 더욱 감소하였으며, $PPAR{\gamma}$, UCP-2, HMG-CoA reductase의 경우 농도가 $200{\mu}L/mL$일 때 각각 35%, 57%, 54%로 5가지 발효 삼정환 중 가장 높은 억제율을 나타내었다. 이에 지방분화 억제 효과를 가진 삼정환을 발효시키면 그 효과가 더욱 증가하는 것으로 나타났는데, 특히 Lactobacillus plantarum으로 발효한 삼정환은 $PPAR{\gamma}$, UCP-2, HMG-CoA reductase의 유전자 발현조절을 통해 지방 분화를 억제시키는 것으로 밝혀져 발효 삼정환은 항비만 혹은 항고지혈증 약물로 개발 가능성이 있는 것으로 사료된다.